• Journal of Digital Convergence
• /
• v.17 no.1
• /
• pp.443-447
• /
• 2019

Aryl hydrocarbon receptor (AhR) is the master regulator of xenobiotics metabolizing enzymes (XMEs). AhR is activated by aryl hydrocarbons upon binding then goes into the cell nucleus and acts as a transcription factor. Despite the role of AhR in human physiology has been investigated for a long while, it is yet to be understood mainly due to the lack of appropriate chemical agents. Furthermore, it has been reported that AhR is related to a wide range of pathogenesis. In addition, recent studies suggest that the study on the development of AhR antagonist may provide a valid therapeutic agent. Some known antagonists in current use are partially agonistic whereas a pure antagonist is still absent. In this study, two phenyl-ring structures of phenyldiazenylphenylpicolinamide has been modified into various structures and evaluated its impact on the AhR antagonistic activity to elucidate the structure-activity relationship.